Mepartricin

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Mepartricin
Mepartricin A.png
Clinical data
AHFS/Drugs.com International Drug Names
ATC code
Identifiers
  • (19E,21E,23Z,25Z,27E,29E,31E)-Methyl 34-((2S,3S,4S,5S,6R)-4-amino-3,5-dihydroxy-6-methyltetrahydro-2H-pyran-2-yloxy)-1,3,5,7,9,13,37-heptahydroxy-17-(5-hydroxy-7-[4-(methylamino)phenyl]-7-oxoheptan-2-yl)-18-methyl-11,15-dioxo-16,39-dioxabicyclo[33.3.1]nonatriaconta-19,21,23,25,27,29,31-heptaene-36-carboxylate
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard 100.057.786 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C60H88N2O19
Molar mass 1141.359 g·mol−1
3D model (JSmol)
  • CNc1ccc(cc1)C(=O)CC(O)CCC(C)C3OC(=O)CC(O)CC(=O)CC(O)CC(O)CC(O)CC(O)CC4(O)CC(O)C(C(=O)OC)C(CC(O[C@@H]2O[C@H](C)[C@@H](O)[C@H](N)[C@@H]2O)/C=C/C=C/C=C/C=C\C=C/C=C/C=C/C3C)O4
  • InChI=1S/C60H88N2O19/c1-36-18-16-14-12-10-8-6-7-9-11-13-15-17-19-48(79-59-56(74)54(61)55(73)38(3)78-59)33-51-53(58(75)77-5)50(71)35-60(76,81-51)34-47(69)30-45(67)28-43(65)26-42(64)27-44(66)29-46(68)32-52(72)80-57(36)37(2)20-25-41(63)31-49(70)39-21-23-40(62-4)24-22-39/h6-19,21-24,36-38,41-43,45-48,50-51,53-57,59,62-65,67-69,71,73-74,76H,20,25-35,61H2,1-5H3/b7-6-,10-8-,11-9+,14-12+,15-13+,18-16+,19-17+/t36?,37?,38-,41?,42?,43?,45?,46?,47?,48?,50?,51?,53?,54+,55-,56+,57?,59+,60?/m1/s1 Yes check.svgY
  • Key:GVEVTKSEPQUIJA-PLDHRHJXSA-N Yes check.svgY
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Mepartricin is a macrolide polyene compound that is useful for urethra, prostate, and bladder function. It has been studied for use in treating chronic pelvic pain syndrome and benign prostatic hyperplasia. [1] [2]

Pharmacodynamics

Mepartricin is an estrogen reabsorption inhibitor that may interfere with the reabsorption of estrogens in the gut leading to increased fecal estrogen excretion. It reduces 17β-estradiol concentration in enterohepatic circulation and decreases estrogen levels in the prostate. The effect of mepartricin on the reabsorption of estrogens was evaluated in studies in vitro and in vivo.

Mepartricin significantly improves pelvic pain and quality of life compared with the results in placebo group after two months of treatment. [1] Regarding to the theory that hormonal disorders could promote prostatic inflammation, [3] mepartricin, that can lower estrogen levels in prostate, is an effective drug in the treatment of patients with chronic pelvic pain syndrome [4] and is referred in 2015 World Journal Pharmacology Updates on therapies for chronic prostatitis/chronic pelvic pain syndrome.

Related Research Articles

<span class="mw-page-title-main">Interstitial cystitis</span> Medical condition

Interstitial cystitis (IC), a type of bladder pain syndrome (BPS), is chronic pain in the bladder and pelvic floor of unknown cause. It is the urologic chronic pelvic pain syndrome of women. Symptoms include feeling the need to urinate right away, needing to urinate often, and pain with sex. IC/BPS is associated with depression and lower quality of life. Many of those affected also have irritable bowel syndrome and fibromyalgia.

<span class="mw-page-title-main">Prostatitis</span> Medical condition

Prostatitis is inflammation of the prostate gland. Prostatitis is classified into acute, chronic, asymptomatic inflammatory prostatitis, and chronic pelvic pain syndrome.

<span class="mw-page-title-main">Prostate</span> Gland of the male reproductive system in most mammals

The prostate is both an accessory gland of the male reproductive system and a muscle-driven mechanical switch between urination and ejaculation. It is found only in some mammals. It differs between species anatomically, chemically, and physiologically. Anatomically, the prostate is found below the bladder, with the urethra passing through it. It is described in gross anatomy as consisting of lobes and in microanatomy by zone. It is surrounded by an elastic, fibromuscular capsule and contains glandular tissue as well as connective tissue.

<span class="mw-page-title-main">Benign prostatic hyperplasia</span> Noncancerous increase in size of the prostate gland

Benign prostatic hyperplasia (BPH), also called prostate enlargement, is a noncancerous increase in size of the prostate gland. Symptoms may include frequent urination, trouble starting to urinate, weak stream, inability to urinate, or loss of bladder control. Complications can include urinary tract infections, bladder stones, and chronic kidney problems.

Pudendal nerve entrapment (PNE), also known as Alcock canal syndrome, is an uncommon source of chronic pain in which the pudendal nerve is entrapped or compressed in Alcock's canal. There are several different types of PNE based on the site of entrapment anatomically. Pain is positional and is worsened by sitting. Other symptoms include genital numbness, fecal incontinence and urinary incontinence.

Glomerulation refers to bladder hemorrhages which are thought to be associated with some types of interstitial cystitis (IC).

<span class="mw-page-title-main">Urinary retention</span> Inability to completely empty the bladder

Urinary retention is an inability to completely empty the bladder. Onset can be sudden or gradual. When of sudden onset, symptoms include an inability to urinate and lower abdominal pain. When of gradual onset, symptoms may include loss of bladder control, mild lower abdominal pain, and a weak urine stream. Those with long-term problems are at risk of urinary tract infections.

<span class="mw-page-title-main">Polyestradiol phosphate</span> Chemical compound

Polyestradiol phosphate (PEP), sold under the brand name Estradurin, is an estrogen medication which is used primarily in the treatment of prostate cancer in men. It is also used in women to treat breast cancer, as a component of hormone therapy to treat low estrogen levels and menopausal symptoms, and as a component of feminizing hormone therapy for transgender women. It is given by injection into muscle once every four weeks.

<span class="mw-page-title-main">Estramustine phosphate</span> Chemical compound

Estramustine phosphate (EMP), also known as estradiol normustine phosphate and sold under the brand names Emcyt and Estracyt, is a dual estrogen and chemotherapy medication which is used in the treatment of prostate cancer in men. It is taken multiple times a day by mouth or by injection into a vein.

Prostatic congestion is a medical condition of the prostate gland that happens when the prostate becomes swollen by excess fluid and can be caused by prostatosis. The condition often results in a person with prostatic congestion feeling the urge to urinate frequently. Prostatic congestion has been associated with prostate disease, which can progress due to age. Oftentimes, the prostate will grow in size which can lead to further problems, such as prostatitis, enlarged prostate, or prostate cancer.

<span class="mw-page-title-main">Acute prostatitis</span> Serious bacterial infection of the prostate gland

Acute prostatitis is a serious bacterial infection of the prostate gland. This infection is a medical emergency. It should be distinguished from other forms of prostatitis such as chronic bacterial prostatitis and chronic pelvic pain syndrome (CPPS).

<span class="mw-page-title-main">Chronic bacterial prostatitis</span> Bacterial infection of the prostate gland

Chronic bacterial prostatitis is a bacterial infection of the prostate gland. It should be distinguished from other forms of prostatitis such as acute bacterial prostatitis and chronic pelvic pain syndrome (CPPS).

<span class="mw-page-title-main">Chronic prostatitis/chronic pelvic pain syndrome</span> Medical condition

Chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS), previously known as chronic nonbacterial prostatitis, is long-term pelvic pain and lower urinary tract symptoms (LUTS) without evidence of a bacterial infection. It affects about 2–6% of men. Together with IC/BPS, it makes up urologic chronic pelvic pain syndrome (UCPPS).

Urologic diseases or conditions include urinary tract infections, kidney stones, bladder control problems, and prostate problems, among others. Some urologic conditions do not affect a person for that long and some are lifetime conditions. Kidney diseases are normally investigated and treated by nephrologists, while the specialty of urology deals with problems in the other organs. Gynecologists may deal with problems of incontinence in women.

<span class="mw-page-title-main">Estradiol undecylate</span> Chemical compound

Estradiol undecylate, also known as estradiol undecanoate and formerly sold under the brand names Delestrec and Progynon Depot 100 among others, is an estrogen medication which has been used in the treatment of prostate cancer in men. It has also been used as a part of hormone therapy for transgender women. Although estradiol undecylate has been used in the past, it was discontinued and hence is no longer available. The medication has been given by injection into muscle usually once a month.

<span class="mw-page-title-main">Gynecomastia</span> Endocrine system disorder of human male breast

Gynecomastia is the abnormal non-cancerous enlargement of one or both breasts in males due to the growth of breast tissue as a result of a hormone imbalance between estrogens and androgens. Gynecomastia can cause significant psychological distress or unease.

The side effects of bicalutamide, a nonsteroidal antiandrogen (NSAA), including its frequent and rare side effects, have been well-studied and characterized. The most common side effects of bicalutamide monotherapy in men include breast tenderness, gynecomastia, feminization, demasculinization, and hot flashes. Less common side effects of bicalutamide monotherapy in men include sexual dysfunction, depression, fatigue, weakness, and anemia. Bicalutamide is well tolerated and has few side effects in women. General side effects of bicalutamide that may occur in either sex include diarrhea, constipation, abdominal pain, nausea, dry skin, itching, and rash.

The pharmacology of estradiol, an estrogen medication and naturally occurring steroid hormone, concerns its pharmacodynamics, pharmacokinetics, and various routes of administration.

Urologic chronic pelvic pain syndrome (UCPPS) is ongoing bladder pain in either sex, chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS) in men and interstitial cystitis or painful bladder syndrome (IC/PBS) in women.

References

  1. 1 2 De Rose AF, Gallo F, Giglio M, Carmignani G (January 2004). "Role of mepartricin in category III chronic nonbacterial prostatitis/chronic pelvic pain syndrome: a randomized prospective placebo-controlled trial". Urology. 63 (1): 13–6. doi:10.1016/j.urology.2003.08.006. PMID   14751338.
  2. Erickson BA, Schaeffer AJ, Van Le B (2008). "Chronic prostatitis". Clin Evid (Online). 2008. PMC   2907954 . PMID   19450305.
  3. Fan S, Hao ZY, Zhang L, Chen XG, Zhou J, Zang YF, Tai S, Liang CZ (2014). "Increased chromogranin A and neuron-specific enolase in rats with chronic nonbacterial prostatitis induced by 17-beta estradiol combined with castration". Int J Clin Exp Pathol. 7 (7): 3992–9. PMC   4129011 . PMID   25120776.
  4. Cohen JM, Fagin AP, Hariton E, Niska JR, Pierce MW, Kuriyama A, Whelan JS, Jackson JL, Dimitrakoff JD (2012). "Therapeutic Intervention for Chronic Prostatitis/Chronic Pelvic Pain Syndrome (CP/ CPPS): A Systematic Review and Meta-Analysis". PLOS ONE. 7 (8): e41941. Bibcode:2012PLoSO...741941C. doi: 10.1371/journal.pone.0041941 . PMC   3411608 . PMID   22870266.